Chem. Sci. 2023, 14 (48), 14092-14099
DOI: 10.1039/d3sc05121h
Denisenko A.; Garbuz P.; Makovetska Y.; Shablykin O.; Lesyk D.; Al-Maali G.; Korzh R.; Sadkova I.; Mykhailiuk P.
Bicyclo[2.1.1]hexanes have been synthesized, characterized, and biologically validated as saturated bioisosteres of the ortho-substituted benzene ring. The incorporation of the 1,2-disubstituted bicyclo[2.1.1]hexane core into the structure of fungicides boscalid (BASF), bixafen (Bayer CS), and fluxapyroxad (BASF) gave saturated patent-free analogs with high antifungal activity.